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A Simple and Expedient Procedure for the Preparation of Gabapentin Lactam (2-Aza-spiro[4,5]decan-3-one)
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2016-09-19 00:00:00 , DOI: 10.1021/acs.oprd.6b00246 Jashuva V. P. Katuri 1, 2 , Vadiraj S. Ekkundi 1 , Kuppuswamy Nagarajan 3
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2016-09-19 00:00:00 , DOI: 10.1021/acs.oprd.6b00246 Jashuva V. P. Katuri 1, 2 , Vadiraj S. Ekkundi 1 , Kuppuswamy Nagarajan 3
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A novel process has been described on 100 g scale for the preparation of gabapentin lactam which is a penultimate intermediate for the preparation of gabapentin, comprising a Hofmann reaction of 1,1-cyclohexanediacetic acid monoamide using chlorinating agents such as trichloroisocyanuric acid, sodium dichloroisocyanurate, 1,3-dichloro-5,5-dimethylhydantoin, and N-chlorosuccinimide, which have not been employed so far for making this molecule. Reactions done in aqueous alkali on the 1,1-cyclohexanediacetic acid monoamide led to a solution of gabapentin sodium salt which on heating led to the formation of the gabapentin lactam in good yield.
中文翻译：
加巴喷丁内酰胺（2-Aza-spiro [4,5] decan-3-one）的简单简便的制备方法
已描述了一种100 g规模的制备加巴喷丁内酰胺的新方法，该方法是制备加巴喷丁的倒数第二个中间体，该方法包括使用氯化剂（例如三氯异氰尿酸，二氯异氰尿酸钠）与1,1-环己烷二乙酸单酰胺进行霍夫曼反应， 1,3-二氯-5,5-二甲基乙内酰脲和N-氯代琥珀酰亚胺，到目前为止尚未用于制造该分子。在碱水溶液中对1，1-环己烷二乙酸单酰胺的反应产生加巴喷丁钠盐的溶液，该溶液在加热下以良好的产率形成加巴喷丁内酰胺。
更新日期：2016-09-19
中文翻译：
加巴喷丁内酰胺（2-Aza-spiro [4,5] decan-3-one）的简单简便的制备方法
已描述了一种100 g规模的制备加巴喷丁内酰胺的新方法，该方法是制备加巴喷丁的倒数第二个中间体，该方法包括使用氯化剂（例如三氯异氰尿酸，二氯异氰尿酸钠）与1,1-环己烷二乙酸单酰胺进行霍夫曼反应， 1,3-二氯-5,5-二甲基乙内酰脲和N-氯代琥珀酰亚胺，到目前为止尚未用于制造该分子。在碱水溶液中对1，1-环己烷二乙酸单酰胺的反应产生加巴喷丁钠盐的溶液，该溶液在加热下以良好的产率形成加巴喷丁内酰胺。
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